Name: Octreotide acetate
Synonyms: C07306; D00442; D02XIY; L000453; AC1L8LCD; AN-15653; gtpl2055; AM034456; DR003664; drg-0115; STL483734; LS-177735; sm 201-995; octreotide; sandostatin; san 201-995; sms-201-995; longastatin; sms 201,995; CHEMBL262746; sandostatine; NCI60_025753; c5h12o2.c4h10; AKOS026750549; SCHEMBL678434; octreotide-lar; sandoz 201-995; sandostatin (tn); octreotidum [latin]; octreotida [spanish]; octreotide (usan/inn); octreotide acetate salt; octreotide [usan:inn:ban]; pentaazacycloicosane-4-carboxamide; zacycloicosane-4-carboxamide acetate; 2: PN: EP1358890 TABLE: A claimedprotein; 1: PN: EP1118336 SEQID: 1claimed protein; 14: PN: DE10147056 PAGE: 40 claimedprotein; 17: PN: US6268342 SEQID: 18 claimed protein; 1: PN: WO2005007122 TABLE: 22 claimed protein; 25: PN:WO2007081792 SEQID: 40 claimed protein; 11: PN:US20030229017 PAGE: 13 claimed protein
CAS Registry number: 83150-76-9
Molecular Formula: C49H66N10O10S2
Boiling Point: 1447.228°C at 760 mmHg
Flash Point: 829.053°C
Refractive index: 1.673
Density: 1.395
Appearance: white powder
Description: Octreotide is a long-acting somatostatin analog indicated for symptomatic control in acromegaly and gastroenteropancreatic tumors. Other potential uses under investigation include diabetes, psoriasis and Alzheimer's disease.
Uses: Antisecretory (gastric).
Biological Function: Octreotide acetate, a long-acting octapeptide analogue of somatostatin, has a half-life of approximately 100 minutes. A comparison of the primary structures of octreotide and somatostatin suggests little similarity, but from earlier work at the Salk Institute it was known that not all the residues in somatostatin were necessary to elicit its full biological activity. Other studies suggested that the essential fragment for its activity was the tetrapeptide Phe7-Trp8- Lys9-Thr10. These earlier studies helped in the design of the potent drug now known as octreotide acetate. This drug suppresses the secretion of gastroenteropancreatic peptides, such as gastrin, vasoactive intestinal peptide (VIP), insulin, and glucagon, as well as pituitary GH. Furthermore, it is more potent than natural somatostatin in inhibiting the release of glucagon, insulin, and GH.
Clinical Use: Octreotide acetate is used by SC injection in the palliative treatment of patients with metastatic carcinoid tumors, which are tumors of the endocrine system, GI tract, and lung (gastroenteropancreatic). Carcinoid tumors secrete increasing amounts of vasoactive substances, including histamine, serotonin, bradykinin, and prostaglandins. Octreotide acetate inhibits or suppresses the release of these vasoactive substances and, thus, is useful in treating the severe diarrhea, facial flushing, and wheezing episodes that accompany carcinoid tumors. In addition, it finds use in the palliative management of VIP-secreting tumors (VIPomas, usually pancreatic tumors). Patients with VIPomas suffer a profuse, watery diarrhea syndrome, and octreotide acetate is able to help by decreasing the release of damaging intestinal tumor cell secretions. Octreotide also helps to reduce hypokalemia by correcting electrolyte imbalances.
An excessive secretion of GH from the pituitary can cause the disorder known as acromegaly, which is characterized by a progressive enlargement of the head, face, hands, feet, and thorax. Inasmuch as octreotide acetate is able to decrease the secretion of GH from the pituitary, it is used in treating patients with acromegaly who are unresponsive to previous pituitary radiation therapy or surgery. It is used in the treatment of acromegaly, because it reduces the blood levels of both GH and insulin-like growth factor-I (IGF-I). The long-acting repository form of octreotide acetate also is used in treating acromegaly, carcinoid tumors, and VIPomas, but in monthly depot injections.
Octreotide for IV injection is used in the treatment of acute bleeding from esophageal varices. Variceal bleeding occurs in about half the patients with cirrhosis of the liver and is responsible for about one-third of deaths in these patients. Octreotide is a potent vasoconstrictor that reduces portal and collateral blood flow by constricting visceral vessels, which leads to reduced portal blood pressure and decreases the bleeding.
Veterinary Drugs and Treatments: Octreotide may be useful in the adjunctive treatment of hyperinsulinemia in patients with insulinomas (especially dogs, ferrets). Response is variable, presumably dependent on whether the tumor cells have receptors for somatostatin. Octreotide may also be useful in the diagnosis and symptomatic treatment of gastrinomas in dogs or cats. It may be of use in the treatment of acute pancreatitis, but more research is needed before it can be recommended for this use in veterinary patients.
關(guān)鍵字: 原料藥與中間體;
一般項目:第二類醫(yī)療器械銷售;針紡織品及原料批發(fā);服裝復(fù)試批發(fā);日用百貨銷售;家用電器銷售;第一類醫(yī)療器械銷售;化工產(chǎn)品銷售(不含許可類化工產(chǎn)品);五金產(chǎn)品批發(fā);計算機軟硬件及輔助設(shè)備批發(fā);化妝品批發(fā);消毒劑銷售(不含危險化學品);專用化學產(chǎn)品銷售(不含危驗化學品);個人衛(wèi)生用品銷售;金屬材料售;醫(yī)用口罩批發(fā);日用口罩(非醫(yī)用)銷售;醫(yī)護人員防護用品批發(fā);衛(wèi)生用品和一次性使用醫(yī)療用品銷售;勞動保護用品確售;合成材料銷售;飼料添加劑銷售;藥物檢測儀器銷售;制藥專用設(shè)備銷售;財務(wù)咨詢;信息咨詢服務(wù)(不含許可類信息咨詢服務(wù));技術(shù)服務(wù)、技術(shù)開發(fā)、技術(shù)咨詢、技術(shù)交流、技術(shù)轉(zhuǎn)讓、技術(shù)推廣;染料銷售;衛(wèi)生用品銷售;建筑裝飾材料銷售;電子辦公設(shè)備銷售;針紡識品銷售;貿(mào)易經(jīng)紀;銷售代理;國內(nèi)貿(mào)易代理(除依法須經(jīng)批準的項目外,憑營業(yè)執(zhí)照依法自主開展經(jīng)營活動)。許可項目∶食品經(jīng)營(銷售預(yù)包裝食品);貨物進出口;藥品進出口;進出口代理;技術(shù)進出口(依法須經(jīng)批準的項目,經(jīng)相關(guān)部門批批準方可開展經(jīng)營活動,具體經(jīng)營項目以審批結(jié)果為準)。